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Budesonide
Brand Names/Synonyms
- Bidien
- Budeson
- Budesonide, Pharma
- Cortivent
- Desonide
- Desowen
- Entocort
- Entocort Ec
- Micronyl
- Preferid
- Pulmicort
- Pulmicort Nebuamp
- Pulmicort Respules
- Pulmicort Turbuhaler
- Rhinocort
- Rhinocort Aqua
- Rhinocort Turbuhaler
- Spirocort
- Tridesilon
Brand Name Mixtures
- Entocort Enema 0.02 Mg/Ml (Budesonide + Sodium Chloride)
- Symbicort 100 Turbuhaler (Budesonide + Formoterol Fumarate Dihydrate)
- Symbicort 200 Turbuhaler (Budesonide + Formoterol Fumarate Dihydrate)
Chemical IUPAC NameNot Available
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| º¸°ü»ó ÁÖÀÇ |
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| Á¶Á¦½Ã ÁÖÀÇ |
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 | ½É»çÁ¤º¸ |
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 | ÇмúÁ¤º¸ |
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| Ç׸ñ |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
[»óÈ£ÀÛ¿ë/º´¿ë±Ý±â°Ë»ö]
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| Mechanism of Action |
Budesonide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ The exact mechanism of action of budesonide in the treatment of Crohn's disease is not fully understood. However, being a glucocorticosteroid, budesonide has a high local anti-inflammatory effect.
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| Pharmacology |
Budesonide¿¡ ´ëÇÑ Pharmacology Á¤º¸ Budesonide is a synthetic corticosteroid used in Crohn's disease to decrease the symptoms and inflammation associated with the disease, especially at times of flare up. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first pass elimination. The formulation contains granules which are coated to protect dissolution in gastric juice, but which dissolve at pH >5.5, ie, normally when the granules reach the duodenum. Thereafter, a matrix of ethylcellulose with budesonide controls the release of the drug into the intestinal lumen in a time-dependent manner.
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| Metabolism |
Budesonide¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
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| Protein Binding |
Budesonide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 85-90%
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| Half-life |
Budesonide¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.0 and 3.6 hours
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| Absorption |
Budesonide¿¡ ´ëÇÑ Absorption Á¤º¸ Absorption is complete following oral administration.
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| Biotransformation |
Budesonide¿¡ ´ëÇÑ Biotransformation Á¤º¸ Following absorption, budesonide is subject to high first pass metabolism (80-90%). In vitro experiments in human liver microsomes demonstrate that budesonide is rapidly and extensively biotransformed, mainly by CYP3A4, to its 2 major metabolites, 6b-hydroxy budesonide and 16a- hydroxy prednisolone. The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.
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| Toxicity |
Budesonide¿¡ ´ëÇÑ Toxicity Á¤º¸ Single oral doses of 200 and 400 mg/kg were lethal in female and male mice, respectively. The signs of acute toxicity were decreased motor activity, piloerection and generalized edema.
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| Drug Interactions |
Budesonide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Itraconazole The imidazole increases levels/effect of budesonideKetoconazole The imidazole increases levels/effect of budesonide
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Budesonide¿¡ ´ëÇÑ Food Interaction Á¤º¸ A mean delay in time to peak concentration of 2.5 hours is observed with the intake of a high-fat meal, with no significant differences in AUC.
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| Drug Target |
[Drug Target]
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| SNP Á¤º¸ |
Name:Budesonide (DB01222)
Interacting Gene/Enzyme:T-box transcription factor TBX21 (Gene symbol = TBX21) Swissprot Q9UL17
SNP(s):rs2240017 (C Allele)
Effect:Improved response for long-term asthma treatment
Reference(s):Tantisira KG, Hwang ES, Raby BA, Silverman ES, Lake SL, Richter BG, Peng SL, Drazen JM, Glimcher LH, Weiss ST: TBX21: a functional variant predicts improvement in asthma with the use of inhaled corticosteroids. Proc Natl Acad Sci U S A. 2004 Dec 28;101(52):18099-104. Epub 2004 Dec 16. [PubMed]
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| Description |
Budesonide¿¡ ´ëÇÑ Description Á¤º¸ A glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis. [PubChem]
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| Drug Category |
Budesonide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-inflammatory AgentsBronchodilator AgentsCorticosteroidsGlucocorticoids
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| Smiles String Canonical |
Budesonide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCCC1OC2CC3C4CCC5=CC(=O)C=CC5(C)C4C(O)CC3(C)C2(O1)C(=O)CO
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| Smiles String Isomeric |
Budesonide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCC[C@H]1O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@@]2(O1)C(=O)CO
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| InChI Identifier |
Budesonide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C25H34O6/c1-4-5-21-30-20-11-17-16-7-6-14-10-15(27)8-9-23(14,2)22(16)18(28)12-24(17,3)25(20,31-21)19(29)13-26/h8-10,16-18,20-22,26,28H,4-7,11-13H2,1-3H3/t16-,17-,18-,20+,21-,22+,23-,24-,25+/m0/s1
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| Chemical IUPAC Name |
Budesonide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. BUDESONIDE[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.2[SGOT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGPT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0
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